ATM/ATR

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ATM/ATR Signaling Pathway Map

ATM/ATR Signaling Pathways
Isoform-selective Inhibitors

ATM/ATR Products

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  • ATM/ATR Inhibitors (21)
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Catalog No. Product Name Information Product Use Citations Product Validations
S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Cell Death Dis, 2022, 13(2):146
S1092 KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nat Commun, 2022, 13(1):360
Cancer Res, 2022, canres.2229.2021
Elife, 2022, 11e70518
S1570 KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
EMBO Rep, 2022, 23(2):e53658
Cell Rep, 2022, 38(2):110216
Microbiol Spectr, 2022, e0188121
S2245 CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.
G3 (Bethesda), 2020, 4;10(5):1585-1597
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(11):110522
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Nat Commun, 2021, 12(1):245
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.
Ann Transl Med, 2021, 9(19):1500
Drug Dev Res, 2021, 10.1002/ddr.21905
Pharmacol Res, 2021, 166:105459
S7050 AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.
J Med Chem, 2022, 65(5):4182-4200
Sci Rep, 2022, 12(1):5827
Nat Commun, 2021, 12(1):4856
S7136 CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Aging (Albany NY), 2021, 13(8):11705-11726
mBio, 2020, 11(1)
Mol Cells, 2016, 39(12):869-876
S7693 Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Cancer Cell, 2022, S1535-6108(21)00662-0
Dev Cell, 2022, 57(5):638-653.e5
Cancer Res, 2022, canres.1707.2021
S8007 VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
EMBO J, 2022, 10.15252/embj.2021108599
FASEB J, 2022, 36(3):e22221
Sci Signal, 2022, 15(715):eabh2290
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Nat Commun, 2019, 10(1):5718
Nat Commun, 2019, 10(1):3585
Oncogenesis, 2019, 8(7):38
S8096 Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.
NAR Cancer, 2022, 4(2):zcac012
Mol Cell, 2021, S1097-2765(21)00390-7
Mol Cancer Ther, 2021, 20(9):1561-1571
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Cell Rep, 2022, 38(2):110216
Sci Rep, 2022, 12(1):5827
Nat Neurosci, 2021, 10.1038/s41593-021-00923-4
S8556 AZ31 AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S8666 Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Clin Cancer Res, 2021, clincanres.1010.2021
Cancer Res, 2021, 81(18):4676-4684
Cancer Discov, 2021, 11(2):362-383
S8680 AZD1390 AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
Cancer Cell, 2022, S1535-6108(21)00662-0
Nucleic Acids Res, 2022, 50(5):2700-2718
Cell Rep, 2022, 38(2):110216
S8729 AZ32 AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
S9639 VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
J Med Chem, 2022, 65(5):4182-4200
Sci Rep, 2022, 12(1):5827
Nat Commun, 2021, 12(1):6813
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Phytomedicine, 2022, 98:153958
Bone, 2022, 154:116262
Cancer Cell, 2021, S1535-6108(21)00659-0
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Cell Death Dis, 2022, 13(2):146
S1092 KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nat Commun, 2022, 13(1):360
Cancer Res, 2022, canres.2229.2021
Elife, 2022, 11e70518
S1570 KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.
EMBO Rep, 2022, 23(2):e53658
Cell Rep, 2022, 38(2):110216
Microbiol Spectr, 2022, e0188121
S2245 CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.
G3 (Bethesda), 2020, 4;10(5):1585-1597
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(11):110522
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Nat Commun, 2021, 12(1):245
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.
Ann Transl Med, 2021, 9(19):1500
Drug Dev Res, 2021, 10.1002/ddr.21905
Pharmacol Res, 2021, 166:105459
S7050 AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.
J Med Chem, 2022, 65(5):4182-4200
Sci Rep, 2022, 12(1):5827
Nat Commun, 2021, 12(1):4856
S7136 CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Aging (Albany NY), 2021, 13(8):11705-11726
mBio, 2020, 11(1)
Mol Cells, 2016, 39(12):869-876
S7693 Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Cancer Cell, 2022, S1535-6108(21)00662-0
Dev Cell, 2022, 57(5):638-653.e5
Cancer Res, 2022, canres.1707.2021
S8007 VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
EMBO J, 2022, 10.15252/embj.2021108599
FASEB J, 2022, 36(3):e22221
Sci Signal, 2022, 15(715):eabh2290
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Nat Commun, 2019, 10(1):5718
Nat Commun, 2019, 10(1):3585
Oncogenesis, 2019, 8(7):38
S8096 Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.
NAR Cancer, 2022, 4(2):zcac012
Mol Cell, 2021, S1097-2765(21)00390-7
Mol Cancer Ther, 2021, 20(9):1561-1571
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Cell Rep, 2022, 38(2):110216
Sci Rep, 2022, 12(1):5827
Nat Neurosci, 2021, 10.1038/s41593-021-00923-4
S8556 AZ31 AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S8666 Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Clin Cancer Res, 2021, clincanres.1010.2021
Cancer Res, 2021, 81(18):4676-4684
Cancer Discov, 2021, 11(2):362-383
S8680 AZD1390 AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
Cancer Cell, 2022, S1535-6108(21)00662-0
Nucleic Acids Res, 2022, 50(5):2700-2718
Cell Rep, 2022, 38(2):110216
S8729 AZ32 AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
S9639 VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
J Med Chem, 2022, 65(5):4182-4200
Sci Rep, 2022, 12(1):5827
Nat Commun, 2021, 12(1):6813
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Phytomedicine, 2022, 98:153958
Bone, 2022, 154:116262
Cancer Cell, 2021, S1535-6108(21)00659-0
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
Tags: ATM inhibition | ATR inhibition | ATM kinase activation | ATM kinase assay | ATM protein kinase | ATM signaling pathway | ATM inhibitor drugs | ATM tumor | ATM phosphorylation | ATM targets | ATM cancer | ATM activity | ATM inhibitor clinical trial | ATM inhibitor review